Albuterol Sulfate - Albuterol Sulfate syrup prescribing information
INDICATIONS AND USAGE
Albuterol Sulfate Syrup is indicated for the relief of bronchospasm in adults and children 2 years of age and older with reversible obstructive airway disease.
DOSAGE AND ADMINISTRATION
The following dosages of albuterol sulfate syrup are expressed in terms of albuterol base.
Usual Dosage
Adults and Children Over 14 Years of Age:
The usual starting dosage for adults and children over 14 years of age is 2 mg (1 teaspoonful) or 4 mg (2 teaspoonfuls) three or four times a day.
Children Over 6 Years to 14 Years of Age:
The usual starting dosage for children over 6 years to 14 years of age is 2 mg (1 teaspoonful) three or four times a day.
Children 2 to 5 Years of Age:
Dosing in children 2 to 5 years of age should be initiated at 0.1 mg/kg of body weight three times a day. This starting dosage should not exceed 2 mg (1 teaspoonful) three times a day.
Dosage Adjustment
Adults and Children Over 14 Years of Age:
For adults and children over 14 years of age, a dosage above 4 mg four times a day should be used only when the patient fails to respond. If a favorable response does not occur with the 4-mg initial dosage, it should be cautiously increased stepwise up to a maximum of 8 mg four times a day as tolerated.
Children Over 6 Years to 14 Years of Age Who Fail to Respond to the Initial Starting Dosage of 2 mg Four Times a Day:
For children over 6 years to 14 years of age who fail to respond to the initial starting dosage of 2 mg four times a day, the dosage may be cautiously increased stepwise, but not to exceed 24 mg/day (given in divided doses).
Children 2 to 5 Years of Age Who Do Not Respond Satisfactorily to the Initial Dosage:
For children from 2 to 5 years of age who do not respond satisfactorily to the initial starting dosage, the dosage may be increased stepwise to 0.2 mg/kg of body weight three times a day, but not to exceed a maximum of 4 mg (2 teaspoonfuls) given three times a day.
Elderly Patients and Those Sensitive to Beta-adrenergic Stimulators:
The initial dosage should be restricted to 2 mg three or four times a day and individually adjusted thereafter.
CONTRAINDICATIONS
Albuterol Sulfate Syrup is contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.
ADVERSE REACTIONS
In clinical trials, the most frequent adverse reactions to albuterol sulfate syrup in adults and older children were:
Percent Incidence of Adverse Reactions in Adults and Children (6-14 Years of Age) | |
Reaction | Percent Incidence |
Central nervous system | |
Tremor | 10% |
Nervousness | 9% |
Shakiness | 9% |
Headache | 4% |
Dizziness | 3% |
Hyperactivity | 2% |
Excitement | 2% |
Sleeplessness | 1% |
Disturbed sleep | <1% |
Irritable behavior | <1% |
Dilated pupils | <1% |
Weakness | <1% |
Cardiovascular | |
Tachycardia | 1% |
Palpitations | <1% |
Sweating | <1% |
Chest pain | <1% |
Ear, nose, and throat | |
Epistaxis | 1% |
Gastrointestinal | |
Increased appetite | 3% |
Epigastric pain | <1% |
Stomachache | <1% |
Musculoskeletal | |
Muscle spasm | <1% |
Respiratory | |
Cough | <1% |
In clinical trials, the following adverse reactions to albuterol sulfate syrup were noted more frequently in young children 2 to 6 years of age than in older children and adults:
Percent Incidence of Adverse Reactions Noted More Frequently in Children 2 to 6 Years of Age Than in Older Children and Adults | |
Reaction | Percent Incidence |
Central nervous system | |
Excitement | 20% |
Nervousness | 15% |
Hyperkinesia | 4% |
Sleeplessness | 2% |
Emotional lability | 1% |
Fatigue | 1% |
Cardiovascular | |
Tachycardia | 2% |
Pallor | 1% |
Gastrointestinal | |
Gastrointestinal symptoms | 2% |
Loss of Appetite | 1% |
Ophthalmologic | |
Conjunctivitis | 1% |
Cases of urticaria, angioedema, rash, bronchospasm, hoarseness, oropharyngeal edema, and arrhythmias (including atrial fibrillation, supraventricular tachycardia, extrasystoles) have been reported after the use of albuterol sulfate syrup.
In addition, albuterol, like other sympathomimetic agents, can cause adverse reactions such as hypertension, angina, vomiting, vertigo, central nervous system stimulation, unusual taste, and drying or irritation of the oropharynx.
The reactions are generally transient in nature, and it is usually not necessary to discontinue treatment with albuterol sulfate syrup. In selected cases, however, dosage may be reduced temporarily; after the reaction has subsided, dosage should be increased in small increments to the optimal dosage.
DESCRIPTION
Albuterol Sulfate Syrup contains albuterol sulfate, USP, the racemic form of albuterol and a relatively selective beta 2 -adrenergic bronchodilator. Albuterol sulfate has the chemical name α 1 -[( tert -butylamino)methyl]-4-hydroxy- m -xylene-α,α'-diolsulfate (2:1) (salt) and the following chemical structure:
(C 13 H 21 NO 3 ) 2 •H 2 SO 4 M.W. 576.7
Albuterol sulfate is a white or practically white powder freely soluble in water and slightly soluble in alcohol, in chloroform, and in ether per USP definition.
The World Health Organization recommended name for albuterol base is salbutamol.
Albuterol Sulfate Syrup for oral administration contains 2 mg of albuterol as 2.4 mg of albuterol sulfate in each teaspoonful (5 mL). Albuterol Sulfate Syrup also contains the inactive ingredients Purified water, hypromellose, citric acid anhydrous, sodium citrate dihydrate, sodium benzoate, sorbitol solution, strawberry flavor, and FD&C Yellow # 6. The pH of the syrup is 3.2 to 4.2.
CLINICAL PHARMACOLOGY
In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on beta 2 -adrenergic receptors compared with isoproterenol. While it is recognized that beta 2 -adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta 2 -receptors in the human heart existing in a concentration between 10% and 50%. The precise function of these receptors has not been established (see WARNINGS ).
The pharmacologic effects of beta-adrenergic agonist drugs, including albuterol, are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
Albuterol has been shown in most controlled clinical trials to have more effect on the respiratory tract, in the form of bronchial smooth muscle relaxation, than isoproterenol at comparable doses while producing fewer cardiovascular effects.
Albuterol is longer acting than isoproterenol in most patients by any route of administration because it is not a substrate for the cellular uptake processes for catecholamines nor for catechol- O -methyl transferase.
Preclinical
Intravenous studies in rats with albuterol sulfate have demonstrated that albuterol crosses the blood brain barrier and reaches brain concentrations amounting to approximately 5.0% of the plasma concentrations. In structures outside the brain barrier (pineal and pituitary glands), albuterol concentrations were found to be 100 times those in the whole brain.
Studies in laboratory animals (minipigs, rodents, and dogs) have demonstrated the occurrence of cardiac arrhythmias and sudden death (with histologic evidence of myocardial necrosis) when beta-agonists and methylxanthines are administered concurrently. The clinical significance of these findings is unknown.
Pharmacokinetics
Albuterol is rapidly absorbed after oral administration of 10 mL of albuterol sulfate syrup (4 mg of albuterol) in normal volunteers. Maximum plasma concentrations of about 18 ng/mL of albuterol are achieved within 2 hours, and the drug is eliminated with a half-life of about 5 hours.
In other studies, the analysis of urine samples of patients given 8 mg of tritiated albuterol orally showed that 76% of the dose was excreted over three days, with the majority of the dose being excreted within the first 24 hours. Sixty percent of this radioactivity was shown to be the metabolite. Feces collected over this period contained 4% of the administered dose.
Clinical Trials
In controlled clinical trials in patients with asthma, the onset of improvement in pulmonary function, as measured by maximum midexpiratory flow rate (MMEF) and forced expiratory volume in 1 second (FEV 1 ), was within 30 minutes after a dose of albuterol sulfate syrup, with peak improvement occurring between 2 and 3 hours. In a controlled clinical trial involving 55 children, clinically significant improvement (defined as maintaining a 15% or more increase in FEV 1 and a 20% or more increase in MMEF over baseline values) continued to be recorded up to 6 hours. No decrease in the effectiveness was reported in one uncontrolled study of 32 children who took albuterol sulfate syrup for a 3-month period.
HOW SUPPLIED
Albuterol Sulfate Syrup, a clear, orange-yellow liquid with a strawberry flavor, contains 2 mg of albuterol (present as the sulfate) per 5 mL and is supplied in the following containers:
4 fl oz (120 mL) NDC 62135-189-41
16 fl oz (473 mL) NDC 62135-189-47
5 mL Unit-Dose Cup NDC 62135-189-05
20 Unit-Dose Cups of 5 mL each NDC 62135-189-24
20 mL Unit-Dose Cup NDC 62135-189-20
20 Unit Dose-Cups of 20 mL each NDC 62135-189-23
Dispense contents with a child-resistant closure (as required) and in a tight, light-resistant container as defined in the USP/NF.
Store at 20º to 25ºC (68º to 77ºF) [See USP Controlled Room Temperature].
Manufactured By:
Chartwell Pharmaceuticals, LLC.
Congers, NY 10920
Manufactured for:
Chartwell RX, LLC
Congers, NY 10920
Rev 03/2025
L70767
